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HRID 237421作成日:2026年10月24日

Water → 4-{4-[4-(3-Methanesulfonyl-propoxy)-indol-1-yl]-pyrimidin-2-ylamino}-cyclohexanecarboxylic acid methyl ester

https://huagongshe.com/ja/reaction/237421

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物DiisopropylethylamineHCID 81531—
反応物Ethyl 4-aminocyclohexanecarboxylateHCID 409963—
反応物1-(2-methanesulfinyl-pyrimidin-4-yl)-4-(3-methanesulfonyl-propoxy)-1H-indoleHCID 58017086—
溶媒DimethylacetamideHCID 31374—
生成物4-{4-[4-(3-Methanesulfonyl-propoxy)-indol-1-yl]-pyrimidin-2-ylamino}-cyclohexanecarboxylic acid methyl esterHCID 5801709390%

反応条件

温度120 °C

反応手順

4-Amino-cyclohexanecarboxylic acid ethyl ester (550 g) and 815 mL DIPEA were added to 1-(2-methanesulfinyl-pyrimidin-4-yl)-4-(3-methanesulfonyl-propoxy)-1H-indole (746.7 g) in 2.5 L DMA, and the mixture allowed to heat to 120° C. for 4 h and then allowed to cool to room temperature. Water (3 L) was added dropwise and the resulting precipitate was collected by filtration, washed with H2O and MeOH, and dried in vacuo at 48° C. overnight to yield 4-{4-[4-(3-methanesulfonyl-propoxy)-indol-1-yl]-pyrimidin-2-ylamino}-cyclohexanecarboxylic acid methyl ester (90%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08642601B2
出典データセットuspto-grants-2014_02
ORD IDord-756b6cb4452f420ab1aaddc184f78fbc
出典メモuspto-grants-2014_02